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Into a 500 mL round-bottomed flask were added acetondimethylacetate (6.97 g, 40 mmol), acetic anhydride (7.55 ml, 80 mmol), and trimethylorthformate (4.24 g, 40 mmol). The resulted reaction mixture was stirred and heated at 120 0C for two hours, and then was cooled down to room temperature. After removing all volatile material in-vacuo, the residue was dissolved with THF (100 mL), [(4-bromo-2-fluorophenyl)methyl] amine (8.16 g, 40 mmol) was added slowly. The reaction mixture was stirred at room temperature overnight. Sodium hydride (1.92 g, 80 mmol) was added portionwise. The reaction was stirred at room temperature for 30 minutes. LCMS showed that the reaction was complete. The reaction mixture was concentrated, cooled down to 0 0C, and added ethyl acetate (100 mL) and 30 ml of 10percent HCl solution (to adjuste pH of aqueous layer around 2). Two layers were separated, and aqueous layer was extracted with ethyl acetate (75mL x 2). Combined organic layers were dried and concentrated to yield desired product (1.2 g, 8 percent), which was used for next step without further purification.
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